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Compound Detail

CHEMBL397270

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Cc1cccc(C(=O)n2cc(Br)cn2)c1

Basic Information

ChEMBL ID CHEMBL397270
Phase Preclinical
Structure Type MOL
InChI Key WACJMZOPBBWBAJ-UHFFFAOYSA-N
2
Targets
2
Activities
2
Assay Types
1
PK Parameters
8
Publications
0
Known Names

Molecular Properties

265.1
MW (Da)
2.64
ALogP
3
HBA
0
HBD
34.9
PSA (Ų)
0.79
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C11H9BrN2O
MW 265.11
Aromatic Rings 2
Heavy Atoms 15
NP-Likeness -1.84

Activity Summary

IC50 1 meas. best 5.57
Ki 1 meas. best 6.6

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Neutrophil elastase
CHEMBL248
Ki 6.6 6.6 250.0 1
Unchecked
CHEMBL612545
IC50 5.57 5.57 2700.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 5.1 hr -

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Neutrophil elastase Ki = 250.0 nM 6.6 Inhibition of human NE 17850059
Unchecked IC50 = 2700.0 nM 5.57 Inhibition of human pancreatic chymotrypsin 17850059

Literature References

PubMed DOI Target Context # Activities
17850059 10.1021/jm070600+ Neutrophil elastase 1
17850059 10.1021/jm070600+ No relevant target 1
17850059 10.1021/jm070600+ Unchecked 1
17850059 10.1021/jm070600+ Aminopeptidase N 1
17850059 10.1021/jm070600+ Cathepsin D 1
17850059 10.1021/jm070600+ Plasma kallikrein 1
17850059 10.1021/jm070600+ Prothrombin 1
17850059 10.1021/jm070600+ Urokinase-type plasminogen activator 1

Data from ChEMBL 36 via Core Engine